1. Cell Cycle/DNA Damage
  2. CDK
  3. Senexin A

Senexin A 

Cat. No.: HY-15681 Purity: 99.94%
Handling Instructions

Senexin A is a CDK8 inhibitor with an IC50 of 280 nM.

For research use only. We do not sell to patients.

Senexin A Chemical Structure

Senexin A Chemical Structure

CAS No. : 1366002-50-7

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10 mM * 1  mL in DMSO USD 151 In-stock
Estimated Time of Arrival: December 31
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50 mg USD 720 In-stock
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100 mg USD 1250 In-stock
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Based on 2 publication(s) in Google Scholar

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Description

Senexin A is a CDK8 inhibitor with an IC50 of 280 nM.

IC50 & Target[1]

CDK19

0.31 μM (Kd)

CDK8

0.83 μM (Kd)

In Vitro

Senexin A inhibits CDK8 and CDK19 ATP site binding with Kd50 of 0.83 μM and 0.31 μM, respectively and CDK8 kinase activity with IC50 of 0.28 μM. Senexin A inhibits β-catenin–dependent transcription in HCT116 colon carcinoma cells. The induction of transcription factor EGR1 upon serum starvation, followed by readdition of serum, is strongly inhibited by Senexin A in HT1080 cells. Senexin A inhibits only p21-induced transcription but not other biological effects of p21. Senexin A also decreases the expression of many secreted tumor-promoting factors in doxorubicin-treated wild-type HCT116 cells[1].

In Vivo

Five daily treatment of Senexin A fully reverses tumor-promoting effect of chemotherapy. Senexin A shows no detectable toxicity and no significant effects on body weight, organ weights, or blood cell counts in C57BL/6 mice during the treatment. This effect of doxorubicin treatment is completely abolished, however, when doxorubicin injection is followed by administration of Senexin A. Senexin A treatment strongly improves the response of A549/MEF tumors to doxorubicin[1].

Molecular Weight

274.32

Formula

C₁₇H₁₄N₄

CAS No.

1366002-50-7

SMILES

N#CC1=CC=C2C(C(NCCC3=CC=CC=C3)=NC=N2)=C1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 100 mg/mL (364.54 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.6454 mL 18.2269 mL 36.4538 mL
5 mM 0.7291 mL 3.6454 mL 7.2908 mL
10 mM 0.3645 mL 1.8227 mL 3.6454 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (9.11 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (9.11 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
Animal Administration
[1]

Mice: Senexin A toxicity study is conducted by Taconic in C57BL/6 mice, using five mice per group treated with 20 mg/kg Senexin A or carrier (80% propylene glycol), with five daily i.p. injections. Mice are weighed on days 3 and 6, and killed on day 6. Organ weights are determined for brain, kidney, thymus, spleen, lung, and liver. Terminal blood samples are analyzed to determine the numbers of total white blood cells, neutrophils, lymphocytes, monocytes, eosinophils, and basophils[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
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Keywords:

Senexin ACDKCyclin dependent kinaseInhibitorinhibitorinhibit

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Senexin A
Cat. No.:
HY-15681
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